QUINUCLIDINE DERIVATIVES, METHOD FOR THEIR PREPARING, PHARMACEUTICAL COMPOSITION, METHOD FOR TREATMENT AND INTERMEDIATE SUBSTANCES Russian patent published in 2005 - IPC

FIELD: organic chemistry, chemical technology, medicine, pharmacy.

SUBSTANCE: invention relates to novel derivatives of quinuclidine of the general formula (I):

wherein © represents phenyl ring, (C₄-C₉)-heteroaromatic group comprising one or some heteroatoms, naphthalenyl, 5,6,7,8-tetrahydronaphthalenyl or biphenyl group; R¹, R² and R³ represent hydrogen halogen atom, phenyl and others; n represents a whole number from 0 to 4; A represents group -CH=CR⁶-, -CR⁶=CH-, -CR⁶R⁷ and others; R⁶ and R⁷ represent hydrogen atom, alkyl and others; m represents a whole number from 0 to 8; p represents a whole number from 1 to 2; and a substitute in azoniabicyclic ring can be at position 2, 3 or 4 including all possible configurations of asymmetric carbon atoms; B represents the group of the formula i) or ii) wherein R¹⁰ represents hydrogen atom, hydroxyl group or methyl; each R⁸ and R⁹ represents: wherein R¹¹ represents hydrogen, halogen atom, alkyl; Q represents a single bond, -CH₂- and others; X represents pharmaceutically acceptable anion of mono- or polyvalent acid. Compounds of the formula (I) possess antagonistic activity with respect to muscarinic M₃-receptors and can be used in medicine for treatment of diseases wherein muscarinic M₃-receptors are implicated.

EFFECT: improved preparing method, valuable medicinal properties of compounds.

36 cl, 164 ex